Center for Interdisciplinary Biosciences , Technology and Innovation Park, P. J. Šafárik University in Košice , Jesenná 5 , 041 54 Košice , Slovak Republic.
Department of Biophysics, Faculty of Science , P. J. Šafárik University in Košice , Jesenná 5 , 041 54 Košice , Slovak Republic.
Biomacromolecules. 2018 Jul 9;19(7):2459-2471. doi: 10.1021/acs.biomac.8b00057. Epub 2018 Apr 16.
A new gradient copolymer has been synthesized by the living cationic ring-opening polymerization of hydrophilic 2-ethyl-2-oxazoline with lipophilic 2-(4-dodecyloxyphenyl)-2-oxazoline (EtOx-grad-DPOx). The prepared copolymer is capable of assembling in water to yield polymeric nanoparticles that are successfully loaded with an anticancer agent, curcumin. Self-assembly of the copolymer was found to be tuned by the polarity as well as the hydrogen bonding ability of solvents. Solvent took distinctive role in the preparation of unloaded and curcumin-loaded nanoparticles. The stability of the nanoparticles was increased by curcumin loading promoted by curcumin-polymer interactions. Further, the chemical stability of curcumin in water is largely enhanced inside the polymeric nanoparticles. Curcumin-loaded (EtOx-grad-DPOx) copolymer nanoparticles showed excellent stability in the biological medium, low cytotoxicity, and concentration dependent uptake by U87 MG and HeLa cells, which indicate the possibility of their efficient application in drug delivery.
一种新型梯度共聚物已通过亲水性 2-乙基-2-恶唑啉与疏水性 2-(4-十二烷氧基苯基)-2-恶唑啉（EtOx-grad-DPOx）的活性阳离子开环聚合合成。所制备的共聚物能够在水中自组装，生成能够成功负载抗癌药物姜黄素的聚合物纳米粒子。共聚物的自组装被发现可以通过溶剂的极性和氢键能力进行调节。溶剂在未负载和负载姜黄素纳米粒子的制备中发挥了独特的作用。姜黄素与聚合物的相互作用促进了姜黄素的负载，从而提高了纳米粒子的稳定性。此外，姜黄素在聚合物纳米粒子内的水相中的化学稳定性得到了很大提高。负载姜黄素的（EtOx-grad-DPOx）共聚物纳米粒子在生物介质中表现出优异的稳定性、低细胞毒性和浓度依赖性的 U87 MG 和 HeLa 细胞摄取，这表明它们在药物传递方面具有高效应用的可能性。
